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530151 ATGL Inhibitor, Atglistatin - CAS 1469924-27-3 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1469924-27-3C₁₇H₂₁N₃O

Products

Catalog NumberPackaging Qty/Pack
5.30151.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable biphenyldimethyl urea compound that inhibits adipose triglyceride lipase (ATGL) activity (IC50 = 700 nM; [Substrate] = [Triolein] = 165 µM) in a substrate-competitive (Ki = 355 nM) and highly selective manner. Shown to effectively suppress FA/glycerol productions from adipocytes (ICmax = 50 to 100 µM in 3T3-L1-differentiated adipocytes or primary murine WAT cultures) in vitro and in blood of mice in vivo via either oral or intraperitoneal administration (EDmax = 200 µmol/kg) with no significant cytotoxicity up to 50 µM in AML-12 murine hepatocyte cultures. Although TG accumulation in cardiac muscle causes cardiomyopathy, significant Atglistatin level is only seen in liver, white & brown adipose tissues in wt mice 8 h post single 200 µmol/kg oral dosage.



Produced under the license of University of Graz/Graz University of Technology
Catalogue Number530151
Brand Family Calbiochem®
Synonyms3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
References
ReferencesMayer, N., et al. 2013. Nat. Chem. Biol. 9, 785.
Product Information
CAS number1469924-27-3
FormBeige powder
Hill FormulaC₁₇H₂₁N₃O
Chemical formulaC₁₇H₂₁N₃O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetATGL
Primary Target IC<sub>50</sub>700 nM
Primary Target K<sub>i</sub>355 nM)
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.30151.0001 04055977241228

Documentation

ATGL Inhibitor, Atglistatin - CAS 1469924-27-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Mayer, N., et al. 2013. Nat. Chem. Biol. 9, 785.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision29-April-2014 JSW
Synonyms3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
DescriptionA cell-permeable biphenyldimethyl urea compound that inhibits adipose triglyceride lipase (ATGL) activity (IC50 = 700 nM; [Substrate] = [Triolein] = 165 µM) in a substrate-competitive (Ki = 355 nM) and highly selective manner, exhibiting little potency against hormone-sensitive lipase (HSL), monoglyceride lipase (MGL), pancreatic lipase, lipoprotein lipase, or lysophospholipases PNPLA6/7 even at concentrations as high as 100 µM. Shown to effectively suppress FA/glycerol productions from adipocytes (ICmax in vitro and in blood of mice in vivo via either oral or intraperitoneal administration (EDmax50 µM in AML-12 murine hepatocyte cultures. Although ATGL deficiency causes cardiomyopathy in human and ATGL-ko animals due to severe Triacylglycerol (TG) accumulation in cardiac muscle, significant Atglistatin level (>0.2 nmol/g tissue) is only seen in liver, white & brown adipose tissues, and detectable TG accumulation is only observed in liver tissue in wt mice 8 h post single 200 µmol/kg oral dosage.
FormBeige powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1469924-27-3
Chemical formulaC₁₇H₂₁N₃O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesMayer, N., et al. 2013. Nat. Chem. Biol. 9, 785.